DB1976 is a Fully Efficacious Transcription Factor PU.1 Inhibitor

ETS transcription factors mediate a wide array of cellular functions and are attractive targets for pharmacological control of gene regulation. Transcription factors (TFs) are central to many cellular processes and account for 5-10% of genes in eukaryotes. Besides, sequence-specific binding is an obligate step in ETS-mediated gene activation. So...

JBJ-04-125-02 is a Mutant-Selective and Orally Active EGFR Inhibitor

Epidermal growth factor receptor (EGFR) is a transmembrane receptor protein in humans. The discovery of activating mutations in EGFR detected in 10% to 30% of patients with non–small cell lung cancer (NSCLC). In addition, it has revolutionized the treatment of this disease. Until recently, EGFR tyrosine kinase inhibitors (TKI), including...

PS315, an Allosteric PKC Inhibitor Binding to the PIF-Pocket

Members of the protein kinase C (PKC) family are regulated by phosphorylation and by an N-terminal extension of the catalytic domain. In addition, AGC kinases are a group of protein kinases comprising PKA, protein kinase G, and PKC families. They typically have three conserved phosphorylation sites. Besides, all PKCs...

CCT36776 is a PROTAC-based Pirin Protein Degradation Probe

Proteolysis targeting chimeras (PROTACs) are heterobifunctional molecules. It induces rapid and selective protein degradation, via the proteasome. PROTACs contain two different ligands connected by a linker, one portion of the molecule engages the target protein. While the other, attach via a flexible linker, recruits an E3 ubiquitin ligase to...

CM-272, a First-in-class, Reversible and Dual G9a/DNMTs Inhibitor

Therapy of hematological malignancies is undergoing a paradigm shift. It is away from the traditional chemotherapy towards the targeting of proteins driving the cancer phenotype. The novel therapeutic approach relies on the use of epigenetic drugs. It aims to reverse critical epigenetic events underlying human cancer pathogenesis, particularly abnormalities...

Ro 90-7501, a Radiosensitizer, is an Aβ42 Fibril Assembly and PP5 Inhibitor

Cervical cancer is one of the most common cancers among women worldwide. Ro 90-7501 is an inhibitor of the amyloid β42 (Aβ42) fibril assembly. It is associated with Alzheimer’s disease. The usual method for Cervical cancer treatment is Radiotherapy, especially for locally advanced cancer. However, the treatment results are...

CID-1067700 is a Ras GTPases pan-Inhibitor with High Efficacy Towards Rab7

Alteration of small GTPase functions is a hallmark of genetic and sporadic human diseases, making GTPase family members attractive though understudied targets. Specifically, the Ras superfamily of GTPases includes Arf, Rho, Ras and Rab GTPase subfamilies. Besides, they regulate a broad range of cellular processes ranging from membrane trafficking...